Advancing Nature's Sodium Channel Inhibitors

Many companies have tried or are trying to develop drugs that selectively block the Nav1.7 channel in order to bring a new, highly effective analgesic to the market.  Development of drugs targeting NaV1.7 has been challenging however, due in part to the difficulty of achieving adequate selectivity for NaV1.7 over other closely related sodium ion channel isoforms. SiteOne has taken a completely unique approach to the problem, leveraging natural sodium channel inhibitors as a template for the design of potent and selective drugs targeting NaV1.7.

With technology originating at Stanford University, SiteOne identified a means of synthesizing, from scratch, these naturally-occurring blockers.  SiteOne’s other seminal discovery was that, in humans and other primates, NaV1.7 has a unique structure which is exploited to make molecules that are extremely selective in blocking the channel in these species. These compounds act as molecular “corks”, which block NaV1.7 selectively over all other sodium channel subtypes.  Selectivity for NaV1.7 is exquisite, with essentially no block of closely related sodium channels involved in other physiological functions at therapeutic drug concentrations, leading to a block of pain without any appreciable side effects.